Compounds > PI3-Kinase-alpha-Inhibitor-2

PI3-Kinase-alpha-Inhibitor-2 and Neoplasms

PI3-Kinase-alpha-Inhibitor-2 has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for PI3-Kinase-alpha-Inhibitor-2 and Neoplasms

Article	Year
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . Journal of medicinal chemistry, 2008, Sep-25, Volume: 51, Issue:18 Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of PI3 kinase p110alpha. The synthesis, biological activity, and further profiling of these compounds are described. This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer. Topics: Administration, Oral; Antineoplastic Agents; Biological Availability; Cell Line, Tumor; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Humans; Indazoles; Magnetic Resonance Spectroscopy; Molecular Structure; Neoplasms; Phosphoinositide-3 Kinase Inhibitors; Sulfonamides	2008

Article

Year

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Journal of medicinal chemistry, 2008, Sep-25, Volume: 51, Issue:18

Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of PI3 kinase p110alpha. The synthesis, biological activity, and further profiling of these compounds are described. This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer.

Topics: Administration, Oral; Antineoplastic Agents; Biological Availability; Cell Line, Tumor; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Humans; Indazoles; Magnetic Resonance Spectroscopy; Molecular Structure; Neoplasms; Phosphoinositide-3 Kinase Inhibitors; Sulfonamides

2008